HUE033898T2 - CB2 antagonistaként hasznos piridin-2-amidok - Google Patents

CB2 antagonistaként hasznos piridin-2-amidok Download PDF

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Publication number
HUE033898T2
HUE033898T2 HUE13799543A HUE13799543A HUE033898T2 HU E033898 T2 HUE033898 T2 HU E033898T2 HU E13799543 A HUE13799543 A HU E13799543A HU E13799543 A HUE13799543 A HU E13799543A HU E033898 T2 HUE033898 T2 HU E033898T2
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HU
Hungary
Prior art keywords
methyl
cyclopropyl
pyridine
carboxylic acid
amide
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HUE13799543A
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English (en)
Inventor
Uwe Grether
Atsushi Kimbara
Matthias Nettekoven
Fabienne Ricklin
Stephan Roever
Evans Mark Rogers
Didier Rombach
Gasch Tanja Schulz
Matthias Westphal
Original Assignee
Hoffmann La Roche
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Application filed by Hoffmann La Roche filed Critical Hoffmann La Roche
Publication of HUE033898T2 publication Critical patent/HUE033898T2/hu

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    • C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/60—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D213/78—Carbon atoms having three bonds to hetero atoms, with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C07D213/81—Amides; Imides
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Claims (8)

  1. IGÉNYPONTOK 1. (I) Äsllnoi Mpötü vegySlil,
    ahol Ü! jelentése hSÍÓ||§% föiÄÄ&ikoxi. halnfenilalRttj: oaetmólpxl Wosíltei IsalolénUaikoxi vagy aik!löseía?iÍá!köXicsopof|;: K ' jdentésekalogéd dkloalkil. haloazetlÄM-, ksfópdDlidMk vagy Mlöoxddiifösöporíi: RJ és R'* egyike hidrogén vagy kikik 8 másik pedig -(€R5R”M€ R ?R8)«-R?í; vagy RJ m R4 azon nitrogén atommal együtt, amelyhez kapcsolódnak 2-oxo-$~aza·· spvrof 3.4 joktii, hal oazef td m 11 vagy hal op i no! idi ni lesöpör loi al koma k; E® ás R* egymástól Ägetletnl választott a ilvetkgzesök hidrogén. alki, dkioalkiteikik haloalkil, dkloalkil. alkilszoiíhnüaikii, ddnialkozialkik hMroddlki. hdoazeíidmiiaikil, hahazeüdirnlkarbodL 2Haxa“6~az&$pirup3]heptaníik8rhoni!, alktiaptmdkarbooiíí dialkilantínolaipniJ. -mAâîîI azeiidMlkarhonil, oxeíantlaiMI is alkiloxetanil; vagy 11' és Rft azon síénamonnal, együtt. amelyókhez k^Rvsoiidsíák, dklóaJRíii okéhmlit, oxanik vagy dioxotietáoilt alkotnak; R; és R* egymástól független választható a következőkből: hidrogén, álkitékdkloalkil; vagy R?és Rh azon szénatommal együtt, amelyhez kapcsolódnak* etklóalkiit alkotnak; az ld jelentése alktl, alkoxtkarNali» jWÉ$8íö.í». animóharbonik elano. pirtdimh alkilammokarbonil oxazoRkril, Mklj4lJ,4|oxadkzo!~3~il, alkihetrazoltb aHoiüazokMi, I H^eimzol il, S#lkík| 153,4 ja>mdIaioI-2-ik azebdmilkarbonsL haksizetidimikarhoníl, 6~o\admza,spirop.3jheptardk .Menüd I Λ4|-o\adiazol4Ai! vagy hilodÖ«Aöka^p%M:« értéke pedig 0 vagy I; lei téve, hogy amikor mind R:', mind pedig R"’ aikií egyidejűleg, akkor R; és R2 nem tehet mindkettő halogén égy sperret vagy ezek gyogyászatllag ellógadható sója vagy észtere,
  2. 2. Ai'. I. igénypont szerinti vegyük;!, ahoi R: jelentésehaloalkoxí,
  3. 3. Az. I. vagy 2. igénypont szerinti vegyidet ahol R' jelentése írifiuoretoxi, tniluorpropdoxi, dlfiuoretiloxk tlaoretiloxi vagy duorpropiioxi.
  4. 4. At l~3:, Igéhypöntök bármelyike szerinti vegyüíet, ahol R2 jelentése plMoafkli vagy haioazetidinü. Si. Áz 1-4. igénypontói hárPielyike szerinti vegyidet, ahol R2 jeientise ctkioproptl cikiobutH vagy dilluorazetidinii. ót Az 1igénypontok bármelyike szerinti vegyidét, ätnelyhett az R? éMR4 egyike lidzogén., a : másik I RsH*}-( C R ^1¾ , ?, Az A->b.igénypontok bármelyike szerimi vegyüíet amelyben R* és R4 egymástól RiggetienÖl váiasztotidk a következők közül: alkil, eikinalkllaikü, alkilszullbnilaíkil és oiiloalkii, vagy Is és I#ázott szénaiomsnal együtt amelyhez kapcsolódnak, diosotietanilt alkotnak. I, Az 1--2::igénypontok bértnelylli.: szerinti vegyiiet, amelyben RZ és Rz egymástól Siggetienií választottak a következők közül: metél, eikiöpropibnefíl, metiiszulfonilmetil és cikíopropik vagy R5 és R(> azon szénatommal együtt, amelyhez kapcsolódnak, diöMtietanlit alkotnak.
  5. 9. Az 1~8. igénypontok bármelyiké szerinti vegyüíet, ahoi R9 jelentése 5-alkií-[iJAJoxadiázö1-3-il vagy armnokarbonii,
  6. 10. Ax ) -9. Igénypontok bármelyike szerbül vegyüíet, ahol Rv jelentése S-rnetib 11 (2,4|oxadi«zol“3 l! vagy amiaokacbonik 4L Az IHtilflipoftldk feteölpLä saerkű vs||übl| amiben R? és: RÄ ggymdidol ilgptferdU vsiasKtötiaii: &amp; következik közílk íildrogéa, meül és eüí, vagy R/ és iR^iazoo sÄatomkal ®g>4Ats amelyhez kapcsolódnak. eikiopemib vagy ciklohexlíl alkotna!?, !§. At 4-1L :l|énypPîÂÉnti>'e|plbi;Âëtyhea R^éS^é^klejöléféfáik^iiii f|>: Ag 1---42, Igénypontok bármelyike. szeriod vegyiíét, ahol n értéke ö<
  7. 14. Az 1-43:. igényposnok bármelyike szerinti vegyülő* -a következők kílzö:Lkiy|lasztv8; l4|P^|ylöM-|6d#pdin--2-'karoonil)-amino|'2~meüLpropioä^av--meül''bszier; S-Klór-4 -dklopropHmea>xî«pjrî<ltn-2-karbonsa% -rS }--1 ~karhanmîL2-'dkiopfop;lAïtil:L amid;
    5--Rlör“4-fIkioprobimetoxLp|ridio“2:“karbonsav4Rbläy0xi-eikiolie:xilmPd4|'>adtt:d:;:
    5-RjóM--ciklúgfopi|memM“plfldbL2#azbönsa.vAtl^^
    5-Klô^4-eîklûpmpiltpelôKHpit4Â:i2iàarbonsav--{{S}-4”hidi'oximet5L3«- metikbutil}·· amid; JkíiliM-^lklöpfppilmeíöxl^piiilP^ksrböü^^ickpp^lmeilhmeíll^amtd;' S"Br0no4^eiklopropilmMoxi-pinÄ--2'-kadxrnsäv-((R}~]~kart>atrtoiLB'ntetll-4>uti!)--amid; 5-Kléf4-eiMopropilmetoxí*pifldm-2*karbonsav-({S)-1 -hkirox Imetll-1 ,2*dimetll-propi 1)- amid;
    5-K Íór4--eíkIopeöpíImeíox!-'pírídín--2--karböfi4av''((R)·· LbldroxlmeiLS-' metlLpropil)- amid; 5“KI6r^^iiPbö^fe^rf^Mdät*2>liä^Äaav-e)kytMÄjmetik|k2-^t.mötliaptppU|*· amid; l-KMmd-e i klppropl imetöxLpÄii^tetÄMV^R
    5--Klör-4miklopmpimem:xi-p1ry|p--2~karb0psav<-((R)-!-lvld^x;Ím8dLL2>>diníet5}--pföplí)-- amid; S-IO|ml£Jbr444~t1immbemdfpp:ifÄ prop.il )-'am ici: amid: |i*||.ldr4#ÄlöP-P^Ä^^P',T^*n”2^8^n^v”C3“i«droxi“2j2-dim©il^p^pilNÄJ S-Ki6f-4-ôÎklôpH^lteÂX^|^idlm3”Mrbsc}say-|i«{2-hymxl-etil}~2~merij<pfopii}«aipid; 5'Kiôri4wélkiopmpitopm^i«piHdm^^^|ïifpopsasi4î^^i®P^pâP3*hidroxl«propIi)'-âmii; |~Klér^d"p|klaprôpiiP©Â^p3«dm>2-fearponsaV'Pvydrommeî|l^iktepepd!mmll)-aMid; $“Klér'4-©lklopri^ïteetoxPpMPm'-2~kafbos5$âv41~fôtd'-i 4udmxteeffi''pr0pi!)~anïid;
    5-KlöiNl*elfclop^Ift^^pMdiö>Mg^ttsä¥KCS>2Jji^ii{©tvi~pMdlß->Mto'iI)« amid:; S~Kiér»4"Íoxsan-3“ímxi}^iHd!n~2~karboosav-((:Í|~2s2>'dimeiil~Í~meií!karbonmíl~pföpíi)·' amid; S-lOomd-p, 2,2-ari n«ör»©mm)«plrídin--l-káf bbnsav4p)4i4~dimeb I » 1 miabikarbamoil· propilVamki; S- K ldNl^&amp;Np^plil«^t@ilkptrI4|^|“jtol©ps8.vv|| 4« dîm i mati M 3 -d i \ neii I -butii ham id ; S40br4Pk{opropflMmM-^ ! 4bds4Mmtól4 -mëili-propiO-amtd; :54Mb44dklbpKïpi1îMï©m^ I J-dimed]- butíij-sroid; 5'-KI<.P'-4-cddopr<>piimoa;rxii;irí<linN2^k8rbonsavoa2P}-d-d'ddroximeill«ly3-<Hmetíi"b«t.l!}·' anad; :S'vÍ\lbf^4--oikl0p?'opiÍ,nmt0xi'-pl:ridsr^2~k8fbonsaV'4(llj:>i~bldim*Í54aöl"2,2^dimPiibp?4pil^ amid; ::5«^lôr-4~cikU>propilmetoxi«piri<jin-2"karbonisaV"((R)· i midpMlmetn-' i > meubpropd)- amid; MetÍi--3»({(5-kiór“4~(ciklo|ítx>pilmcroxí)pifidtn*2-í)}karhonn^amioo)-2>3-clip^llfeUt^^áf : :S*!Mî'-4«iS i klpplpsl ni ~kaÉ>amakd' i diidPmimsiil 4-:lëi Ι.-bUtä i >* amid; S«íClörf^dik3dpTOpihaaldkii)lidi:ö-2-kaí%onsa^4(^Í''!J4limbbi~2~ madikadiamod-propll^amld; 5“iilôM”Cikl0propi:hïîetoxi -pírtdin^-karbonNavHlR)' -1 <iimèâl-2"Tnet!lkaà*ïiits· prop!) )~am id; S-Kléf"4«dMppí®pílPíetöxl-piÍdín-2#arbDnsavd3»oxas;ol“2“il'í>Jíaíaíi·' 3~U)mmId;
    2-Klöd4*dklbp;qp!fmöM^ -hitoxuiasíil-í ~niötíl'^Uí5l|-amiM;
    5-Klor'4'í2Jd4rifíuor-etoxi>-pindinddarbo?)savd2d~dlaietíkl--tía?o]'-2-'iPpropíl)~ amid; |-®d^4doxeta:adldloxi)-piddm-2~kafbansav-<2,2-dimeUld~tiazoi~2~îPpmpil4-aPùd; P-IClér-d-Cd-llaof-bea^iÍPkippiridia^ferboasawdlSj-l^^^diaof-1-pírMm-d' ll'edíj" amid; ^«Kldr^d'di-insr^benzill-piridin'S-kartensavdiSl-S^^-tfsdyor^i-piridinkl-i^atii^amid· 5~i3iklopi‘opíi-4-c!kiopropilaTetoxi»piridIn~2~karbóasav-(:Uüaaol"2-ií~<me(af^3-if)^annd; 5"C!k1opropíb4<dkiopropiltma<>xs·fiπdiîvd4a1rbonsav22ddimeti5~l·dazol"2di- propd)'-asnid; 5'Cikiopropí Μ-d k íopröpiimeipikpindia-d-karbppaa2^|1^41kldpi'öpll~ MS-meul-I l;2í4]oxadiazol--3~ii)~et.U .{-amid; amid;
    5-Cjkk^ropH~4<iki<3propi!men«xi^vridin-2-karhon^t2>ti2-trifl«^lrpMdm-2-îWi^ amid; ;5"€1kÍ0prí)pi14-cikiopröpiim©toxÍ-fifidli^'2^8íboasa^(($ 1 <k arfeamdtl^;^ ! <buti í )- amid; S-CiklopropH 4 (2,2 i tufmoí-em\d-pirulm 2 k;U'honvn-uSu2 2 dmvíd-i« meti ! karbaraoikpropí 1 Ktmki; 5<dkiopnmi]~4d2,2<24rífm{?T-etoxíVpl5-idin-2»karbonsav~[i -cikiopropH- f»(5- malik [ i ,2,43pxa[||axol^i:1}~etilJ-aT«it|·, 5<1klopropH-4^2<2,24ri0uor“Ctoxr)~piridin-2-k^boosav-(2,2;^iitt!«iM4îÂÎ?l:Hil* propi!)-amid; 5dlΊkioρropi^'4~(2.:2:2'rrs!luoΓ'·e¾κxi}~pirídin~2“karbftnsâV'42,2,2·4ri1]uor''^'pitidin“2“í^' eüíjmmid; 5~i ikiopíopU-4~(2,2>2uriníH>r^nu’<i^pirídín~2-karbonsa\-({SVí4arbaaK'>d-2-nHHil- buídHmid;
    4-C ikk>pfppil meíox i m-Sdtebonsav 41 ->h klrox kn©tj|* eiklopropi íj-amid; 5~C2iklopropb“4-(2,2,2-'ír:i fl a or-eío xi }~p ír ídi m2>karbonsav-; i -éti ! -1 -hid roxi met! kpropíl ρ amid;; :SrOklbp$p:4d2,2,24äflöörÄtKÜtpMdte2NtorböÄ!NIÄdi»xi»)etWkl#4X:ll>^ amid;: 5~(dkiopropii“4»cik;upropí!ineíoxi'plndin'-2''k;!rbov;íiav-(i -h i d ro x \ - e i k 1 open ti 1 meti 1 )~a m i ci ; |:-CÍ:k!opropik4-cikfopmpdmeiuxkpirídin-2~ka#ppsakd'l”Éd?'PXÍ“ eikJbbexilmebi}-- ?anid; :ï'í:ik)opπη>U“4..ci!ciopropäiHlc:ox^ρiπdm·Φk8rbonMf>(¾¾idroxî~ b«ül)-amîü; 54äktppöf4b4--(2,24'4rid^m:~eiOT|pMdm'4dfai^^^^ amid; S"CíikLÍiöpröpi 1 î-mklíspropil-- i-ÇS-ÎTietij- I !,2.4]oxadia^oi~3~îl) ctîi |~aiîiid; S”i4!br-4~(2s2ï2“tîiÊüor~etoxi)“piryiî}:-~2''karboiîsav~[l~0ili!opropfi~l~(l-meîil~ |1,2,# j0Mdls^dbl-il)~dti lj-asmd ; 54 'iktoproßllH -((1^)-2,2.2-4rifi«ört^#lr€te|h!>lrÍám#^#0^V“p-te^iínöi tetib i-i’iüopropd 4-ρν>-Λν\ asdnor- MræUktloxiVpindm-?~kn}'bon\3\-n-karbamoflnîeîü- oxeiaro3di)~aPiid;
    5-Cikiopf»piM-(2s2,2-iritlöii^töM)*pddlft*l*k'ä'rto^a»-t05t)-l-kaÄöaiSil^^il*3-mÄ- bidÉj-amid; 2“(dk.;oprapil'4"i2>2.24.rit1uor~eiox!}-plridish2-kaFb<Mss%í~(íl:i}~'2^cikÍDpmpib i-roebM~ p-madl-} 1,3,4 joxadäa, ok kdK4Ü]-amíd; S-toldopropiM Qí2,24dftwömeíöxppiridfn-2-karboBS#v-[($ }-2-cîkloprop?14«îftêtU* 1 -p" meiií-{! 3i,4|oxadiazol-3-Ui--i.'iii]-'amid; S~€%Ioprppíi“4~((S )--2,2 J>'trii1üemkaaeíd''et0x;i)~pifM{n-'2~körb0nsaV“| Pcíkioproplk i "£S~ e(b[ 1 ^iloMdiazokd-i! }-eti i^appd; 5-¢;ikiopΓopik4H(S^-3-2,24πduofi"mföd!"apκí}~pírIdln4·'karbonsav-[l--cíkiopropfl·j“iS~ «aetU-[ i ,2,4 joxadiazol -3-i IKni l]>amid; 5>-€iklP|p®pi^(^2-liiöPr^«)~piriÄi#)terf^msv4©rc^but|jäm|d) [5'{Jik!opr0pi"4~p<2524rllluor''föfexl)-'pirtófc44ÍÍ~(2-0xa-5~a2í!.“Spíf0Í3.4]okt-'5-dí)~ metánon; S-CikJopropjM ^íR)4>2.2-trifl«or4«mátílk^ötll^lit!Mitó:»kadiíPnsav-'i;í-«'ikíopiOpiÍ-' J* ( 5 ~n kí? U-[ L 2 A ]o>: ad \ axo 1 "3 1 H’tí I }-am i d ; 5>CiklppÄptH4iO*2Jä2^feof4*iföe^ £4dklöp.töpiM~(5-mdti* [ 1.2,4Joxadia;?oí -3-0 j-etín-uraíd; .§-$£ lésM-(2;.3;,2~l:r IRuör-e toxí }-plH6|i-2^r?ÍöSisav ~((S}~ I. -ciki opfopi I -1 -(5 -meii i~ [ ! v2.,4joxc.KÍ ; ázol-3-i.1 }-ed IJ-amíd ; 15“Cik!ppmpil~4-v(2í2,2:4r í Íiiö?»e?oxi)~pirÍd úv-241 j-p S:3~d Iflaor-axoîl d m·~ I ~ íl }-meteöp;;; ! -karlteinoi I- \ -meul-propü)- 5 * < 3 ^ 3 - 01 ft uHf-a-set id J ΐΐ - J -dl >-> 4 > (2,2,2 > t r í fi uö r dSdx i ) >p ! r S <11 d 4iarl>o o sav - ( 1 ~<ïi kldprop 11- í -<>tpgdk[ 1 ,2J|ösíII^oI H--U>-etl j-am Id; 5-{3,3431 J] íáöívpiíMlidln-1 - i ï}~4'·{ 2 d, 2 4r í í lpö^etöxi}~pídd ld-2-fed#dííHv~( !>-clk J:0pröp ! 1-1"{5-ΐ5:50ίΙΙ- [ I Jdjö^adlaz r> i - 3 - i ; H ti ) ) -am id; n>2^foxadia/ol-3-i IjHtl ij-aro í d ;
    5 -Ci k idpropíÍ<'4'd(S)--2,2 > 2 -iriflddr-1 ~med H iox í |^p ifid m-2-karfkmsæy* |2«m£$áhszu 1 fbmí-I -metU-145-roeiií <{ 1 >2H jo.xadkxok>41 }-eti Í J -amId ; M55kl0pföpílH-(2d2v24nnyöp®idxH^^ feutíi}-amíd; 11,2,4 |o xacli aííd- 3 -1 i)-bptll J-amid; S-SikJppröpJl^^l^-íHfJudr^tokO-pyd^-kMto^xp^ítexulfési^ieíi^J^.#* meíii-f i,2(4}osadía?oí~3'iU-t:til Μπ'ϊΙίΙ;
    5-Kjór-4--(252,2--iri si}~arok1; cskfopropil-1 dSmelií-! l,24jo\iüia^oó,Mi}-etíipandd: 5-{ 3,3-! >í iluor-asíeiidin- t-ÜM-{2.2.2~iri iluor-etox n-fdfidin-Z^arbon'un'-jd S}~ i ~ ciklopropí!" ! --{5~meui~i 1 !2.:4|oxadíaxoÍ-3'íi)-etíl]-'amíd; 5-Κ.ΙοΜ-(2<2<2~ΐηΠΰθΓ-ι>!οχΐ)~ρΪΓίλί{π~2·>!ί0ΓΐΗ»η&amp;ίν*[2κ:Ι!νΙορΓ<φΜ!*1*«^ΐ!>»Ν5*ηΐΛ« f ! ,2f4]oxiul kixol - .3 -ín-etií J-am id; 5K33ÄD?:fluör^ttld:i««|:4|^H2Ä2*ö4ß«or<t»Kl|^lÄi^iÄÄS^v«Pke-iW^3pM* safâtil-1-(3 -meid 4 i ^4|px.ad Ι·»^ΜΙ)·^ΐί IJ-äs í d ; 5^3,-:3«D!fter^!eríds]a-t«l|442>2<2''{nfiui>r*etö^|iydlPii2-káirfeo»^»|CE|'2-eiklopr^plí» l-ipodl-I; -i S-metil-[ !2M joxadiazol-3-i!)*eiH]-amid; 5--( 3,3-Ds nuor-ít/cíií!in~i*n )-4-(2,2,2“!riftuor-eioxj)-pirldit3-2-kaffeofíks\?4(S:)-'-2:*· iíyppropH- 1 --meti!·- 1 ~(S-metO~Í 1 ;3>,4]o.x adia?ol"3-ElJ-eîs ! ao^kl; 5-'-Kl0j'''4''(2!2,2"trifiuor''etoxi|-;pifliin~2'-ka^feönsaV'-|i!k)-'2~cskloprppil“I“m4dkk“C2^st|k |L2,4!{í\tu8,3<'o;'^'J'' otd ) amid; ^ Kso ' <, Y' 3 ,! Yiuos oíoxo-pralmY -,,rho^Nav-pSVYct kio'M opd l-ímítd-da^^ötíí· [!,2,4]oxadia/53)-3-ü)-cíHj-amid; 5-433-Di fluorst/oUd««-1 ' il i-4 -(2,2,2 4rifluor"etoxi)--piridin“2'-kaî'bûpsav~p^ ïnelàusxulfonH" \ -metí1-1 -t5~metU'j I J4|oxadia*.okVi !}*e?il]-am4el; 3-i 4 Médium-aactidin-d -iH- 4 ·3 Υ22Υ,2--ΥΠοογ·-I mot Π - mo Y V- p in d i n - 2 - Láb on sav | \ ciklopropíi--1--(3 metΠ··| í ,2,4joxadiaiíöí~3-íi}“etii]"ijmid; 543Íkiopropü-4-(2,2>2~tri flu.d.P*eíoxi )~piriüin~2-karbonsav«{· 1 33~trtmetil*· [i,2s4)oxíídsa^ok3”i!Vhuíií]-amíd; i '(5~metíl'[ 1,2 ^-1 |o s a<1 î au«> l~ 3 »i î )-e i 01 ~a m Id ; S^CIMapropíi-^2J Jlsö^íöKS^^ ;meiá3ipo:l:feíii!-· i -místit * 1. -( 5-;met|l^ [ I ,2,4|<>x4diäiK}k3 '21j^etll|--amlíct j S~C'I klöpfropIl-^^iC^í 2-tr ííí íior^ í -meti í )-p i fid! rí 'S^karlscí ïssgtv io prp|5ii - i ~ met? í~ i ~(5^0»Ι^[ i .2/l)osadiam!”3>'i1}'Stn';-anniU S42lk!o$p^d-4~({SV 2,2, .'Μ π Huívr- 1 -mod keiox Π-pint ímd^karbunxav-pr «jlÆiopropI ! -1-01¾^ i ' M5-mGÜi-( i Z4|u\adur/ok3~ílKíídi'öí0Kd 3„(3<3..1>5fluo^a2&amp;üdin-2-^)-4<(S)--2!2,24rÎi«OT-|^metli«-fêt0xi.î"piridin-2-k:arboBSÂ¥''p>'
    5-Ciki0pfopH^p}“-2j2,2>>Mfiu0f4-i«Ä meiánsxtdfbnik 1 -«jeti í- ! -(5-meid - j ! ;24)oKadia:«sl"3--i!VetiS]-amid; ΐ3θΙε1@ρ?ορΙΜ42ί1^ΐΓΐίΐ9ΜΗδΐΡΐΙ^ίΛΙ^2%^Μ»~(<ΙΙ}~1:^3;4Η:Ρ5§ϊ)Ι-ΐ~(5'β^Ι!!^ f 1.2,'1]o\iKlu/oi-3-iiVb»{íi]-aníld; [ 1,2>4]ox;ui Sazo í -3 - i 1)- bűül] -amid; ^Cddoprapd-d-eikk'pu'p'insetoxbpindin 2d atboa^v4feítd^utH^Íi^qfíB;i'd; 5 ~0 í ktepröpl Μ·*(:2 ,2 *2 dHíí Ä-etoxi )-pirkiin-2-k arte^4#^fewt?i^|il*apiidv 5d2ikk>bu{5l·4H3,2J-"tr!t1uor~¾oχ{}-pírídin“2-karbonsav-·[2-·cikI0pí·opíbi-meü^·^·(5 meül-f ! ,2,4 joxadiazoí-d-ílVeíi! j-amid; 544klobu(ib4d222!2-UMd]iK>rHaoxf}-pirldhi~2~karbonsuv-[20neiá!SSiadr0r!ÍI'd--metiI''l-(5-meíd-{ I f2,4|öxadla^ol^kk4í)^ül]-amiil; 5d.'ik!{4.>utib4-(iS>'2/2«2drî!]uor“!”nKîtiï-etoxl)-piridin~2-'karbô!isav~(2'-clkk>propii-·!-meid- ] -s 5-meükí 1,24!{XKadtax0!~34!)<eíÍij^mkii iPtPd I-f 1 ,2,4] IJ-eil trrfluóMMi)piidrn^24i»böxamM; îrifluer^xl^ààln^-fepbô^PÂ' (SS^-lHP^lM^pöpil^iÉlofí^llmstöxOpíridm^^a^öillH^^liút^icPéÍiáli-S^ karboxatpid' karboxamíd; 5-43tkl obiki-lk-f (2 ll|kl -dikibpropd -2-4 5 - Pi êil-> 1,2,4~ox adkgpká* i!)ppapM-2-di§-4-’( 2,2,2 -trip uoretoxifpirid i n-2-karhoxam id; triOuoretos. s)pindin-2-karhoxam id ; S-Ciku.íbuuí-N-'jPdd-metil-;,2,4-ox&amp;dia?.ol-~3-di)- 1 -motsir>mIfoniipropan- 2-i íj-4-((28)--1,1:,:1 -trí ÍMörpröpan -2--) I ]:oxlp5rídt)t:-2:--kárbdxdíöidt 1 > 1, ! -'UU)«orpropan-2--s i j ox i plri d m-2 -karboxa s a kI ; 5-C2kíobyíü-N-( 1 -eiUopropü-2-í 5-meti i* 1,32^^^4)4^4^141^^31)-2-111-4-((28)-1,1,1--trifi tiüFprppap -2 -i f j o x í p í rid S π-2-karboxamid ; S:-ßikiöbuti:i--N4i -eikiopropil-2:-p-á:VtítfJ:~lJ2,4-öxad1d^k3-í:f)própan~2~IÍ|-4--||2Í}-ly1;!l--trifluorpropsn--2-ii)oxipiridin-'2-'karboxamí(1; (2R)~!-(5--(?ikk>prf^il-4-(2,2í2--t)ídura'etoxl)pMdÍ!n-2-«karbíMídÍ-4,4-dÍfíuorpirrxí)idia-2- karboxanbd:; ood *ol ' il)p ipu 2-slj > í ^hidroxíoxeían-d^l^ i2,2,2-£ril!:uö!X)t^ 'M/'ü'JobnH-X {x '8ρ2~Ρ'ηκη5--!,2 4-*'\ kiszól-' -mcuK'uiftmi-i'iopor» 2 i\\~ 4-(2.2,2“íríHuorí;íox5)p5rídm-2-karhoKasníd; S-CJfcIoteií-N -[{2R )-2^$«roôiil J (2,2>2^trítM^r^@xf)pírtd}n“2~W|pxB.míá; ^iJlyulfonilpropanO-il j-4 J(2S|-1 JJ 4rtî«oïprQ|pH3~2·4Ipöxspíridin-2-k8rb0xami|:;: S -f CH; 1 obuten-4 ~l IJN - Í2 -:5"5BelM,2: I -3 ·ί|)Ί i IsKölíbn î !prîipâri>-3-ï 11^4- (2,2,2~iríf!uoreU>xi4pírldm-2-karboxanűd; í-CiUopropü-NJl-Osí-áíSlu^í'a/oisdíO' i -íí)-2-(5-rt)etíí-i .?J-o\dd3aA}!-^-inpropaii-2-ii|- 4-(2,2J-pjî1uorôetoxi)piridiîî-2~k;jirbtfXu{r5id; 5-< i -i ~ -î 5 ->m ©tjí j” 4-(2,2,2-trifl mm £ί»κί)ρΐ rîdbi Jl'-karbo \aml à; ; {(2SV- ! J J -t»0rpmpi)-2^îj^|piridin4^Â5xam.îàr>; (2>2,2-trífluomoxj)pjridíft*2-karböxmi% 3--(3-JpöroKiÄ^ I:,2,4~oxadia:MClJl)~ I;^nisÉilszûlfônHj|iMp0^ 3-(3-flHot‘oxctán-3-H)-N“({2R}“2-(5-metU-!,2.4-oxad)í«:ob3-U)-1-meUlsxulfonÍ(pfopan-2- ί 1 iriíly ös:e í í é; 'H<l.Ältel«)eiU-3-mcii iszulfoníi-1 -^öpröpan^-iíj-S-cibfepbpíl^-p^J-n i'ílaorot-' \;)pirid5ri-?-karbo v1·' síd: N-| (2R}~1 -cÍkIopfopd-2-(5-meü 1~ ! ,2,4-xmd5öMd-J-] í)propan-2-i 1|-J jB-fluörösgta-SJl}'- 4-(2,2,2 -ír i fiuöföÄi^iryw-2-karb{>xam iá; KJ(2Sí-ï-s£ïildÎ>propí1-'2~l5~í'ííeíí?~lJ,4-Oxadk^c>;'^ CpÎ(3paâv2-î]]-'SJ3--iii0roxeÎan~3'U)- 4 “(2,2 « i i^g:. iN|:!:HÔUiWîk{ôbutiÎ|~M4âKÂ^ü4j^^MdîMôlff3^i)«!HMÔfettife»i.l^!©^»^2-ii-4“ s|,I-tfit]a^-prop8T)i''2~iäjox^ifidfn“24aärbox8ä?üd; S-i î "fl «or©ik lobutil>>^~^^(S^ïïîsstïI~ î t^3-í 1 )~ 1 "met|lsïie«i fbïi î I )-4“ Srlfíi^rétoxDpind in ·· 2 «karboxannd; '5~οϋνΙορΓορ]Ι-Ν-|.(28)-1-Η>ί{ΓθχΙ-2-{5-ηκΗϋ~Ι,2,4-οχ»ίϋα/.ίί)-3~ιΙ)ρΓαρ»η~2-ϋ]-4~(2«2>2- trill uorefôvdp ind in~2 -karboxairnd; N uk'op'oi d \ \2i<> n c iM ? Ss nets' \?*4 ovdhiA.\ * f >M^paa 2 d Í u\2 1 tnflubïëiox^pirid m-2»kafbi sxarnid1; §*b[:|*^kl0p?X>pib24S4$®$H»l>2i3?4o&amp;ad| i(2S}~!x i J~inl1a©rpropan'2:-li|oxip5ridlrp'2>4arbôï48H:ûil:| P»(2<?àdô*!*âiki^ibpiîpt>pian;^i|^;l»iÂbiiMe{M^i1M*K^4sî.,14i&amp;^fbjpâ^ 2-4l]öXipiridin-'2%ar|warnldi btp-cfy opropibi4S~BMi-b s2,4~oxadiäa;ßiM«i!|ab! j>5^p^;uöröx©te^Hii)-4''[P^I* :S«Äfepropii2Ndn bd-p^metib ! ,2>4-osadkK)i-4~ilip!^an-2di 1^442,2- db! »oretoxi)pi rid i?v24aifboxamk! ; 5-cÍfcÍ0pmpií~N-| 1 -cikIopropib2“(|“nisbblp.4-oxadiÂï-3“il}pmpan-2;-yH42-b uorelo xi} pír s din ~2~k a rho x a m i d ; S<ik!opfppi2N4l .»(3. J^áifluomzetidin- i - il}«2*-(S«nieiiM JpböxadteobS »ilbi -oxopfopan'2-i]]-4a;2;2Ja.fii]uori8o>b}paidin4b4arboxamidi 5-oikit»}m'pit-N-[2-c5-mi,id-b2,4~t>xödlazoU3-i!>-1 p-oxa-b- :vaspuoj 3.3|henn.uv· 64i|~j ~oxopKîpan-<2-I|]~4~{2,22*trifiuorsi:Oxi ipiridin^^karboxamld; 1 5»*^«tîl-1 * î î- Î ”*'*xopro|>3o -2 · i2>' 2-tritluoreu>\ifpiridín-2~karboxasrbd; S-dkiopropii-N-f 1-t:iklopïopif-2-(2”medHeti,a?.ol">»ti)prtfp»n'2-j{|~4'i 2.2,2-uiiluore tox i )p i ri d i n - 2 --karboxamkk 5-riMopropü-N -[ i -dklopwpi 1-2-f l-'metlket«j?.ol«S~il)prop8n“^~fl}^2.2«-· Irt f!u ureiox i }p iridi n~2 -ka rfcoxam i d ; §^cík!ppíöpn-l^^[4^d-metil~! J~Uu/ol~2-í!}yxan~4~ir|-4"(2,2;2dr!Íuoretoxl)pírldíPí-Í-ferboxapbd; 5 i-dkf oproplf -N~ [4 ~{5. -mefci 1-Ί ,3 -4iazoU2dl|:os:an-4-511-4 ~(2 ^.^tóííuoretox'íjíjpí rid m~2~ kurboxamk!; 5~cíklppíOipil4^!pl^^;í'-biklopTOpfí-2-(S^me|{Í-:l ;2/4oxa<jiít2ol'3-d')propan-2'il]"4-(2,2·· dífíppretoxilpirídin -2-karboxaroid; í k lo prop i í - N - [ ( 2 S;>»:î -metîï-1 :sí2;i;4“Oxa-cl àlS^Âdxi}pîridin-2-karbo»ud; d'-p|ksoprop!l-ld:-[(3i-)-i^:íklopropIb24541idlfkí:?l54-óxadiMol-l"Í^ fi uorer<>xí)píridi n~2-karboxam ki; 5 ~ e i k i o prop i 1 -N-[(2S}··! -d klopPâplk2-(S -met s I -1. ,2d"Oxadiaxol"3-íí}propan»2-dl~4~(2·' ÍbPímoxi^íridin“2“karböxamÍd; S^dkldpropl l-T&amp;f 1 -efklbptOpü-^-pdPdl-l 5á^daa:0!~2~í! }nropan -22-11} -4-(2,? 2 ' tri H iióretöx S:“dklopr0pí!'N”Íl“G!klopropil'kk-f.ll b;etnmd--5-il)propaH--2--111-4--(2,2,2' tritluoreumtpirkbi«- 2 -karboxauid N~j3~f2-amini>2-oxoetilVf ,l“ílioxotíetan-3-íl]-5-cik!opropjí-4-f2j2*2-ï r i ti uoreioxljp i r i d i n-2-ka rhox &amp; m i d ; 5-C5kÍopropíl-N-[.íx2'diinoPl-l-i ς -neni-L ' --o\adsu/<'l- 5 ihpropü j--í-5 2,2.2- iMfl:uoi»tO'3íÍ||3!í:PÍdi iTítlt3oaMoxj}pirldin-2-karböxam|id:;:·: 5^ífct^frop)l:^~|2,2"íi»«fí|l“l H-"í'^ti1ieír®ol-5~0)pn^y|-4»p52.2-4T'ii1»öreíöKí}p^^®'" 2'-kaFböxaffld( 5-plki^pr{>pyyM~j2p'-dsn)eiÜ-l-|l ~îï^ e Ci 1 tfâira^oî ~5 ~í 1 }prí^il| > 2~ir i ft ti ore îpxlïpï rí êI í ^ " 2--kadx>xamkl; N-[2-(S-amino-Í >2,4~öx;idia/oi~.l-n)-{ •>cikiopropilpmpan*'2~.d)0-‘ c»kk*propH-4r {22,24rífluoreioxi i p i r i di n -2 -ka rbox am kl ; ; N-{{ 1R.}- i -ciklopropik í ~(5 metU - k24-Oxadí azo1 ~3~\; jeíHj-$-{:M]uoroxetan»3dl}~4-· {2,2.2-írif1uorííloxupirföin~2-k8rboxdn5Íd: N ~{ü S}>- ! - g i k feprepk í *( S-mat ií?· i ,2.4'oxad iazo!-> 3 -il)eti i )-5-(3 • duoroxctan-3-dH · (2A2,2«|çii^Qfetoxi )piridla~2d<arboxamíd: N~[ I ~cik)opr0plM-(5-?neü I- i Μ, 1 ^rL0uopm>pan2dl]oxipmdin2-kadxaauxkk N-|l -cikíopropiM -(5-meui- !2/^-oxadía2x>k3~U}eíH]"5-{341uoroxeUm--3“iO~4-4{2S)·· U, ! 4rdIuorpropan~2'íi)oxsp!rsdín--2-karh(>xaiT5Íd; N-| í'Cikiopmp!Í-2-(5--metil- ! ,2>4-oxadia2ol-3-í!}pröpan--2-i!Í-'5--(3·- fluoroxcian- N-j i-ciklopropií~2~(5~mein-!,2,4-oxadiaxol-3-inpropan-2-i!]~5-í3-nuörfíxtítan~3~in-4-[(2S)2, 1, Í4ríl1uorpmp8n-2-íipaxípirldín~2-karboxniníd; 1, ! , 1 ••Î.rifiUorpropan-2-i I joxîpïr.idin-24;arboxamid; J~c!kíopPápl í ~H-| 1 -ssilcio í ~ I I iljpmparí-S -íi 13 (2.2,2- tail uortiU», i )pl rid i n-2 - karboxaimd ; S-dkfopmpi 1 s 4-ox ad I aïsol -2 -1 ]^prs>p i !] - ,2 ' :;tf!^ÎfiSrêîôX'i )jpi r id i η N'-j2;2'-dimety>>l-(5--meül"L3>4--oxadirfzol"2'-il)propii)-5-(3--i'!uoroxet^~3--il}~4-i:(2S)--1, i, Í4|íi^rps%an-2»!l |oxípíod!n--2-kar|jöxaroíl:: :H4^^öp^pt^2~(5~nietiI~]53.4H>xadUiA>l*2-U)pi^p-3-iij-:M3-i1«Srox^rii^M^?4-· ((2S)~ I, !, i -'trilliäorpro'pp-ld! Jox ipi rid m-S-karhoxn; mxl; i-clklopPPpi!í-fíikl0prföpll-2-p''meti!--l3'4la«ötö~U)propM-'2~H]--4^2 J,2~ irilluor^lOxijpirknnd'-karboxaniid; 5^íkliap^píi-H«|'^:!:ííSL-)^-^'S'<Í3metíl-':! “('S^meíííl-1 tri fl í-orcioxi )p J rïdjn-2-kii.rboxaffiid; öt fí aoretox^pf íMírv-2-ksií bPxdîÂ; N-f 1 --aPd«023'.C;3-Piéd Ι-1;:^^«Μϊ^Ι-ΜΙ3ΐ- Î -oxoprópaív5-i!l-5<fkkjpropy-4--(2,2í2-- 5-dkioprapií-N-jl4"ídímeíhandno}~2>{5-metíMí2dl-öxadia£ö}-4MI}-J~ox«pröpan-2''il]~4- (2,2,2-U-í{]uortífoxi)pirídií5-2~kari)Oxainíd; M-| 1 -(axeîidm- í I -1 f2d'OKadlaxöí'l-l|-1-<Mdpt^ ||^2-trÍf1'aorc(Oísi)piríilln-2-karbuxarny; 5^34Íu^xeto«S>:U^~{i~(íTiétiMl«'ö)~2HÍS^éttÍÍ4>2:i4^xM^M~3“l:l)-Í~ö3íPpcöpaft~ 2-111-4-((28)-^, ij I -tîdiï y I oîss pf ítd fí s^S4karb ; 5<ik fopropii-N-l *3 R » - * eikiopíopf ''{^MBetd-í,a>4-C(xadurzol''I-'iI)pR>pa3v241]-'á-{-^'^' d i fi uöretox í Ipsri d i n- 2- karPoxara id ; 5-·c!klopropi^N-·l(2S)-l·dkk>propïí--2--(5~nκîfí^·'l53!4-o^'adiiVXol·2'-iΓ}proρan~2>íl|-'4-·{2,2?2'· tri fi u oreiox i }pi vidi n --2-½ rbox;5 add; 51)5^10-3-0^^5 015 ' )5í55v * <i\OprOfl,5n~2~5'ri-í-\. i kV50>p í * ( ' \?·“ tri fiuofetoxi }pi rid in-2-karboxamid; 5'CÍkK>}iríipi!'N'i('S}' Mn>oùfanôno)'2»{>~inoul· K2,4~oj;aiÍKVokí-i!Ví-í>xo|»o|íiin^S-il];4'(2,2.2-ti1dr!Oî«tox])piriddfe2~k:à#tixâmid; öxopróp0n-2ril3-4“t2,23-trt&amp; i-sMopmpl-^ í~ ! -(metiidrdirid|~ ! .^töpPc^iör24:l!^(252s2- tri ílu orelox S )p i ri din~2-· karfcox ans S d ; 5-cikiopmpiriN'-[2-{5'miíi.)í~ls;k4 -<>xadiaxo!-2-!Í}·· ri-(oxetSív3--il)propan-2-'ii]-4--j’(2S)-· í, !,i4rí11«orprápsB''2-d |pdpi ridín-l-tefboxamidt tri 11 uoretox i }p i ri d ί η··2 - ka? hoxam id ; N-{! ri5''amltt0^! ,2,4-0^4^01-341)-2,2-015^01 ilpröpii)--5--cikíopmpiM-(2,2,2- ilHtlù<^retT3XÎ>i3iiii!iÉ3:i^ri^ri:fëaï%Ô^Îti-ï€l;^ N-(3-;uídní>'d-ciklopröp5Í-í"O\?>pnTd)'>'rik!^pfopil"4-(222t2-tril1u0reri>KÍ|pMdin-2·· karhoxamid; N-n-aj^ino^kMimciU-l-OMvbutajv^-UK^-ciUopropil-d^^^-triHuoretox^pmdjn-í- kafböxaírilál 5-cikíopropd -N-í I -(<iimeüíamioo)-33-d -oxoby Im-2~s! j--1 -( 2,2,2- tri Π uoretox í }ptr I d i n - 3 kit rbcvs a n id, N-j i-(azeÜdm^4!|^,3«ltoefll-ÍHUoh«táá-2rüj-S'«íklbpó|tÍí4-(2,2ji* trUlH^rctiïNî)piridin-2~karbo.xasirid; 5-ciklopa>pii-N-[l-(3,3"dif1u0ra/adidir^d-in-3:3-dÍ5rieú!-l"ó:kobuia55·· 2-il|-442,2:2-tri fi uoretox ?)pi rí d in-2-karboxaot i$; 5''CÍklopropíl'N'{3,3~dimetii'' ! -{6-0x0- i -a za s ρ i ro i 3,3] h ep tars -1-2)- i -ux rdnstao-2-41-4-(2,2,2'tríi'h.ioretoxi)pi.ridin-2-karboxamíd; Ή ·> ( 1 - 4¾ ο^·3 y 3 fötl! ^ ^ àb utÆsn «2 - Il ) -S -ej klopropi Í-4-1 {S?3 J-1 ^ 1 iMHiluorpmpaîi~'·^ U|oxipiriuhî»2-kall>^pïl4|: 3«*UK!optopil.Vv\ íxloneu I kaiotthmimM I oxoNiur»-? - 4'[í?SÍ 1,1" trd:luorpn\p;m~24i]oxipiridin-2-k8rhoxandd; S~eskk>propii-N--[ I -(dimetilaminyikka-dimcdl-l -oxotean«24l|”#~f(2l|~l:VÍ:^1 « trii1uiiipropan-24!]oxipiriciin'2'karboxam!d; NM1 -(azetidin-1 -i Ík3,3-dimetil- I -oxobutan-2 *j 1 j-'d-dklöpropU-d-j (2S >- 1J J ~ trill uo rprppim-S4 ! ] ox i pi ri d ín-2 - k arbox ar ni d: .5~eiklopf»pil~N"{ 1 -(3,3-dil1uofazaddm- \ MI)-3,3-i$m$iM -'OXob»te“24ll~4~[(:2S}~l, ! J~ MÍ«órpróptói-2-iijoxi;pkyin«2-kurlmat»id; wrftiii i- i -i 6-oxa- \ >aziispÄaP#]hep^4^l^##pi^;i|}^« l(2S)~ i, 1,1 -trill ucnpropan--2- i l]ox i pi rid i n«2-karix>x smM; 5-cil* I 114M- f l IM J 2-' d i fc( I !k 1 -< 1 -m©tl i iatra^ol-S-sl jprop ï I ]-'4 - trill uomtoxi )p i fid in-2-k a rix>x ami d ; S-cikiopropn-N-|(iS}-2.2~dimeti!-I-n-;neinis?trazoi--5rii)pmpii]-442>2,2' ^P«MSioxi)pil1:din-2»karhoxamid: N-j(2R)~2~(5-amino··! ;2,4 oxadiazol-3-H}· ! -ciklopropilpropan-M-iil-S- cikiopn>pii-4-p,2(2dri{]upf®tpxi|pifidi?x2«kafboxanrid; N-K2S)"2-(5-anrino-12,4-tíXadiazoÍ(3"i1}-l~eik!ppfopilpröpaO'-2:-iíj~3~oÍkÍoprop!:l'-4~ (2;2,2-írif]uoreíoxi)pu Mm NkatbPMdrid| ί ciklopuvml-N |i Mil ' da xdsl 1 P »»xx lut a ol "< sllptcms pi 2 ? (riűd#j«t0xi)pifídhk2~kark>x'dráid| S->0il£lopi i »pi I"M -[( i S)-.? .2-dîmefy- ! “('iM-rneis lteira^t>l''S-il)pr€ipîïí f^M - (2.2.2-tri fl uoreioxi)p tr i d i n -2-kar boxant id; S--clk!dpropil-M-|( I R)-2,2-dimeui-1 -(5-merii~1 «2,4-oxadiaxol-à-iôpropU j-4 -(2,2,2- 1rs 11 uoretox i )p híd i tv-2--kí trboxam id d-Plklops:opl-N--j {I trifi «ors3|ô^:l )p |ii:iliÎ-2~k8 rbox amid; N~11 ~C5-amino·· I Jpl-ox adsaaíd-3-bI}-2j-dlniebiproplí5-cIklopsopíl-4 -j (2S)~ ,|ÿ! -t r i fládrpr opaß“3 -i))ox i p i ri d i si -d-karboxassijd; f*osklöp.rópi4x-[2(2s4isoeÉf4:~(5--o54ik^ irsnuorpmpan--2-di]oxipsrídin-^2-karboxasii;d: S-eiklopmpiM-fiJ-ipppipMlas^-S-ilfffieloxl^^ 2-dl]pMÉm*2-ka&amp;oxamid; 5~cikií':mropl!"Nd4 3-iBPtlUsíraKo!'-Sdl)propiÍÍ'44(2S}'k! J^i^nfiuorfröpäs-s-2»! l]oxi p i rid s i:K?."karbox asrs ki : 5»cildopmpi !~N '| 2s2~drisattbl~(l~s«dblbíSmxa!~.54|)propíi]-'4~[{2S H J J -mduorptopaír-2-1 ) ) ox s pki d i s -2~karboxamli;:: N~f I ~f S-armoo-- I .d.k-oxadsaxoi-Bdlp-dJ-disnessipsxipOI'-S'-cikiopropil-d-((28)- U J-triiïuorpropan -2--11 joxipiridm-2-kark5xamfd; M-f I *{5-amino-1<2.4~oxadiáról-3-HV2,2-dím^dlpppl!]--5-oíklöp?x)pil·4·>|·(2S>·> 1 * I s ί -íniuaípropio~2-i 1 ]ox ípiridin -2-karboxamid; 5--c;klopropd-N-[2,2-4000111--1-(5-5: seb 1--1,2,4-044411440 i-3~i))propii 1-44(28:(4,4,. (-irs fl uofprop®-2- i Ijoxs p s ridin-2-karbox« id; triiluoi^fôpasi-S-illoxipirHlioxl-karb^Â’nÿv !M'-p-'C2~sm;SBö-f-oxoeíil:)oxéiáo-á-4i|M--(űildopsx3piibiotöxl}-5''C2J~diÍddra^addio-l-s 1 spir id i n--3 -k a s'boxarrs id ; N(-)3--22--3551100-2--0^00111)0^18^^--31-111--5432341510050^00015^-1--15)-4-(2.2:2--tr!f1uoreioxi)pi?id!r5--2-kgrboxamid; 5-dklopropi i-N 4( 2S)-33"d«npiiii» i r i fl uo relax i }p ] rid i n -2-ka rboxa m id : Scikkspr«)pi Î-N Ί « 2RV3%34oneiil~ i-(metilaminoVl-<)\oh«t»n~M|r4-><S»2,2-udl m o\>v3·« tdes ' xerixaamkl 1N“|{ 1 il" 1 *($Mino- 1 tÄU0i!e«to,xi}p'iriclin“2"karh«)xami<l: N-i ( LS ? -1 -(5-iÎiTïm<3^| -3-iOIs trs iluër®töx i ) p ir i di rs -2-karixrxarîvki; :5i 1*1 ΐίpropl!->N-1(2 R>-1 -c äkIßprssp I --metil t«tms^l'S-i!)prripas^^ trill uoroetox i }pi ridin -l-karboxamid; $*blkJ©pfo pü-N«|2-éikl opropi ifl.fiua^ioxi^ N'< 4»am ino ~2 »e ikiöprppllrd-'oxo b«ían~2~ í l}-S-cikbpmpil-4-(2,252.- MfítsöréS^ 5<ík1opropif~N~| 2-trífluofel0xi)p>rídin«2~ karboxaírbd;: 5-cíklopropH~N-[3-|2-(meiU8min0)-2-ox«ctíl]oxetan-3-H]~4~[(2S}-1}I!l”inntíorpropan-2-yjPMlpifíd in- 2-karbox amid; 5~(?k3~dibuomxetidii5-1 -ü)-N-(3-f 2-í meüiammo)-2-oxoebí joxeuai-3-ií j-4-í2 ,2,2-tri ilnnretoxilp;ridiít~2~karboxafníd; 5-blk:bpr«pi-N~p~(3~duorprópi!kárM^ si}?ntttoxí[pií'idíí)-2'karböxasnid: N-[3-(j3«K!ór-2-t1uorpiOpii3kíirbíiTT5on]peíitasv3-ií]-5HdklopropjM-[(3-rneiiioxeui0-3- ii)n>eioxiipindia-2-karboxanPd; S-n ikl öpixspf Ι-M- [3 - h idrox i.-3-œedM.~(meti laPii no|- i -0X0feötap^Wíl|i4- 5-eí.k1opropH“N-[3-fluof-3''metiH''{metHam{no)-«l~oxob«tan>2~nj*4~{2,2>2- tritliiöíxíiox ) }pi rk1 I»-2“|ax teplä; S^ellílöpöpi 3~iüdroxi~3-rnet|!>>;l ^{mtliíáMÍ3M}^4 > ! J- tfiÍHorprp>3n-2~ii]ox|píridín^2~kafbox8m|Í:; N-(isaîttiœ«33'-^^®îi:i- !^5Mhutan'2~U >--5"CÍkiopropí j-4-j (IS)-- l,i J ~ínfluorprttpan~2~ íljoxipirídmtó-2-karhoxaroid; M-(l~amibö-33-(liMbtii-]:-bscöfe:útar^2'dl)^S:<!Möpropi!'44Pi)"^^. 1 •triíluorpropan-l-Si |ox i pírul i π-2-karboxa m id ; .5-aíklöpröpU-N-[(2S)-2-dkÍöpropíl'4-(metHamiaóHH>xobupff“2!*í|H'*{2,2J*‘ trinuomoxi)pindin-2-Uarboxamid; 5~cik!opro|.d i-N~[(2R)-2~cskíopropiM~(niatíiamíno)^l'-oxoboian-2-'S|]^i-{2,2.2--ifi llPPi'PiOkí)pír5dlp"2'-kar boxám id : N · [(2S )-4“amippl;^Möpmpll-»4*0X0bp|^i-2^I^$“e:iMpp!Kaji{M^2Ji“. îrifl«oretoxi}psndm-2-karhoxamid; N-|(2R}~4"amíiío~2~cikk>pa>pii-4-oxobm«in· 2- d { 5"Cikioproptl-4-(2,2>2-irí fluoreto s:i)pirid in-2-1-:arboxamid; 5~c;SkiP:pmpSi~bi''{'{S4r;aiikddia-4-<x\adiaxo!-2“il}'-(>aH'sS!oxeian-'3-'Si)meiS!|-4"{2>2,2'' i f i Π uoretox i }p irid in-2~kar boxarn id ; 5-cik!opropii-N-{{ 5-met Si - i Jul-oxadiazoí-d-i 1 )-(3 -metí ioxcîan-3-il)meHI]-4~ j(2S)~ U J-triiluorpropan-2~ü|oxipi rid in-2-karboxam id ; 5-ciklopropii-N'|2-cSklopfopil-4-(metiiamino)-'4-pX0bpmp-2-fi]-4-{(3SV|,|J" trí Hu orpropan-2-i i]o>; ípíritíi η - 3-karboxanud; N-(4-aakifK>~2-c.íklo].nx>:bl-4-öXf:4pítan'2-ilf-5-cikíopropií~4-l42S)- SfI J-irifiuorpropaïî-2' ÍI{oxipSridÍ!>~2-karboxamid; 5<ik!o|>fopH~Ni-[2‘Ciklopropii«4«(melUsfiiiiino)“4-«#ii^uta;n~2“ii'|'4-((2Shl»l>i ' ΐπΠϋοφΐ«Ρ®η-24ί]οχίριπ&amp;η-2^8^οχ8ΐηίά; >cikíopmpH4sJ2Mkinpropib4^neuiamiuer4'Pxobunm~ >-T|-4..[(2Sî- MJ-tril1uorprôpsrx2~J]oxipindm-2~MrbMMp!i; N-{2-amino-1 -(3 -meiiloxetap-:3^ii|:-2^xöp|iMJ-cikbpropi 1-4-1(28)-1 J J 4ktf!t3b?|impaPi' 2 4 ; )ox ipi rid in ~ 2 -k arboxandd; 5 -c! k Ippppil-N - [ 34bi drox i -3 -met ii-1 -(ntepldmmo)-1 *ùmb\ ita n~2 ~i 1 j *4 ~ {Í 2 S H ? U * ' tri !4yprprdpdP;-2-lli|Dxlpii4ái d-2 - kaeboxatn i d ; J^ikipp^pll:>M-|3^hifex!:-3-meu!-1-(metiiaPdnD}-l-0xobutan-2 -il1J J -ânorpropasxS-i! foxlplr! íiisx2i4íarboxam id ; 5«e3kiopmpií-N-[(5''metií-l?2í4-oxMiaxo!-3-il|-3~metiIöxeian-3-i]3nteíi!|-4-[(2S:p;I,:l;:|·- p4i1«orpropan~2-i ! loxiptridln-2-kar boxamid ; :5-eikiopropii~N-IX$-meb:i-l::j;s:4-oxM:iaxoi-3'iil|-:(3-'ty3etiIoxetap"3J:13metii|Mi|(2S;|“:i:J.1;- bdtlMp^ropaP-2;4j]oxipiM ! ~à ni i n i ï-3,3 -d í n tet i ) -1 -oxoboiar4|4t|#~{3,3-d i 0 uorÿEet i di π-M î}-4-|Iî2,2-iriiPmreioxOp iridié -2 4; a rho x a mid ; d)piridiî'5~2-karboxam i d ; lj-44-aPiÍ3bxI:^:iÍippröpib4^xobi!tan-2'-S:!3-:3-aikIop3'ppik4-|(2S)-! »triiöä^^an^-i ί; J jöxí pl ridíí|ii^34^^feöis-ip^ N~{4 -8ínino-2~cikiopropH-4-oxobutaU“2-i !)~5-e ikiopropiM-j (2S )- l,hl 4fi0uorprtm4nÆ iijoxipíridin-2-karboxamid; 'N-|Y2R)-l-aimno»3Jb-dimetjl:-i:-pxôbutn»-2-iij-4deiklr!propibnstox:5)-3-C3d3-*# Spórádét i d i n 1- ü ψ i ri d i n - 2 -k arboxmpid ; H-|pi;p| «&amp;m i η o -3 3-d i met i ! - :ii -nxnbntatn2 xlli|-4-(ei klppr opt lmetoxi)- 5 -{3,3 - B~jpR}~t^jp04j4imeíU^ 1 ~i |}«4^γ252-.2~ irrnuoreürxi}psrkMn-2-kafbo.Kamkl; :iN|"|'(2S)-l~a{tíino-3f3-dii'neíi^l-oxobutan~2“ii|'5-(3J-«dinuorazeí}dí«~l-iI}-4-(2,2>2~ irh1uoreioxi)psr'k1ln'-2-karbox;;innd; N»|3-(2~ííniinu~2síxoetirhU kKra)xotíetan~:k'iij-'5C3í3-di.0uorazeildin-i 41)-4-(2,2,2--tri duoretoxi }pi rid:in~2-ksrboxam.id ; ,1 -d|öxötiÄi-P4!^^ iritkK^ropan-24ljoxipiridln-2-karboxams<k ï, I ^l-tdiporprdpatt- ^^i^osípiryin-i-'feafexaptdt M-p'-(2~atódö-2^Me£t]}“ 1 , I -dtoxotiëÎsnP-ill-d-CcikiopmpiliSéiex^P-pp-d) fi pdf axsiidia- 1 àl ; ^~|i{ 1 PÇ3 <tii iexetsnP ~I|P“OXdeti i IP-ciy ppropl I~4~{2.2S2- i ri 0 uoreiox i )p i r id i n-2- karboxamid ; N»(i ! SKü-amino- \ -(3-mcu lo\etan»3- d}-2»oxoetil1'5·οΐ:^ρρκφΙΙ··-4»<1^'2*. tfîÛ!Uoreloxi}pindju-2“karboxamuk H~[{2S}p^minoP-cík!oprípdí-4'OxobutanP-íriP-<?kiöpropii-^-(2-fluo®íoxi)pMdmP<· ksrhoxamid; N4(2!p-4vamIno4<Íkiopfopd-#ox:0buían^P-di|-5^tkIöpropb4d2-Í:UOfeí:okt|p:Íríd}P-2- karboxapTid; N-Í(2SÍ~4-ammo~2~cikÍ0pmpb-4-fíköbPtaa-:Níf-S4bk^ 2-karboxamid; N"[(2E}~4^ami.no-'2~cikiopfopl:“4"Oxobpt8a-2;d!j''$''Cikbpmpîb4~(2J>' di Ouoreun \ s p i r s di η -3 -ka dx a as i d ; NM .3~(2-8mmo~2'0>;öeíí!)' ! J"dioKf}Uetan*3-il)-5“Cikiopmpil'4-{2.2Hliß«iöÄj^{)pirl8|p¥': 2-karboxamid; H~f(2S)"4*^j»ino-2~ciklopropiM^?íobuíaH*>2-j|}«5-{3,3”difiU#|í8zetiá!iri4»U}"4-(2,2>2- tritlooretííxDpirídin-'S-kaifepxaírfid: N'{(2Rí-4-xíni>'mí-2-v.'ikU>pfopii-4.íixob\5t8n-2"iíl ~ <s3 .'»dinutsfa^otidin-i-íl 1-4-^,2.2-tr4lui‘íeloxí)pírklVn--2--karhox8m;d; ltd íl uörpsxípanvd-5:||í3xí ρ I dd hi^2-kaí-fexam leír ίτΐίΐ .u oíiprappt --2>-i||pji|pi rid s n -2-ka rhox a m s d ; S ~c'î k i s2j4-oxai|É^1~Í“ll)w,Í"· îïjeti ls^ltbniiprppâîï*24i)pM|l^t%fl3ô»M; 5-€5kiopropiM''-C2''i]u0reioxi)-'N'!(2$|-'2»(5--n^dl-vi,2>4<-ö*alia%bIr34id-maii k&amp;rboxam i d ; K j 3 a 2 -ammo -2 -oxoeûi)-1, í -dlaxut îftan-^-U ]-5-cikiopropi M~(2-f!uoreîo\i }pindio--2-karboxamid; 5-xdklopr§p!:#H3»P*i|í^^ tritlaore(.0xi}piridin'-2~karboxaaiid; <Β}^^^ΐ!Ρρ»ρΜΝ4Κ2»2^ίίΐΜόί^ιΙ)2ΐ|,.(2*{1Ν«ΐ{|ΐ-» I ^^ladías^l^-il)-1 -(metiis2uiibnil}propan-2-'d}pikoäiuamid; (R)-5~dklopropi 1-4-12.2~dU1uoraloxi i-!k-PHÍ-Pi abb!,2,4-oxad kixol-3-ii)-I - (mad bau ίίοηΙΙ)ρΓαρ&amp;«··2··Ι !)píkolinaroid; 5-< l -il\«ôrtîîÎ!?k>buiil)-'N-'{'3''f2~(metUammo}--2-oxoeUri~ i, 1 ~dk>xouctaii-3~H}-4-(2,2,2-biSiioruioxs)piridin»-2--iarb0xainld; N-p--{2'amino-2-0xoedl)-1,1 -•dioxöfePín-'SdlI-S-'Cií --lluprciidobut i) )-4-(2,2,2- tríf!uoretox0p?rít5m-2-karboKamïd; 5"CÍklopí'opíl'N--{(R ^t-eiklopro|>H”2~<5»vneUi~i>2,4"«xadia7oî-3*H)propaîi^."'li)-4-i|p)4~ Éporpropan dMio.b }pikof mamiid! S-cÄpropnb4-((S)-l>>ofklöppopik2Ni>))leiil>db^ ï - íí mtptopm “2" i loxt )plkof lkam Id' : 5··οΙΙί1ορΓορΐ!·Ν··((Κν·Ι»ο;Κ1ορΓθρί1*·2-·(5··η'!<4ΐ1-·1ΐ2!4~οχ4^ίίΐ^ο!ο-ΐ1}ρΓορϋίν2·ί])·4··((Κν 1 ÄPiproptoS 4!öx1 jpskoünamid; § - c ik όρ 11-N -( (S)-1 iíöpi I - 2-( s-m^tí ί- l:52j4Peadbzol^341}jir^paß»2“IH*f!^H;“ fiuorpropan~2-Uoxi}pikofmami4f il]oxipirym»2«karhi>xamid; :l^~|;B'-(2''aaTf0ö'^:>'Oxoeisf}~li!~<lbxoiki8a"34l]“$-eikioprppy-4-[(2R}-:i#iäpp5rop§p^-: ii joxipindin -l-karboxam ki; N'{4-amino--2-c}kiopropu-4'Oxobuuin-0“?fV5<ik)opmpfl^4P)"bIuörpföpäP~2-> íJóKs)pbo!ina5Pk1; $fN[4“ä8 « i οα-2-cik lopropí i <4hgm&amp;BÏ«^ ( f 1)-1-11 ií0ipppa«~2~ dl:px!)plkö!ffiaíPli; 5-cikfopropl! -4-((8) - ! 4luorpröpaa“2“ifoNÍ)”N“i(S)~2-{5-írMf-)2w4"OkadIá'«íí-2-ii)'·!-(mot Hasul ion i 1 jpropan-2 - i 1 ) p i k o ! i namki; S-cíkíopropíl~4~{(S)"{"jliaírproprai")"iíoxi)-N-uíl)-245^®tíl'kl,2s4H'>^“día:íof~3-iI)-'1' (m«tHs/uiAfnii)prtip;sn".',-inpíkoHnön\!<k 5”Ctklopropü-4~((R)‘I dhjofpmpam»&amp;-i on-) \ f-anai2 1,2.i-oxana/oM^ii' k- (rn ctü szu I fon i 1 )p ?x»pan -2-il )p ikoiin arw i d ; ^'CikiopriípiM-uRH-íluoqírupatv^-ibvn'N-uíD-^.'wnuíí'í ,2.4'0\adia/ui' 1 il)-|)WPtîlMÂwCW0Pan"2»il)pikolinaitild; 2443-(2i, I-I loxoipia^ íTÍf]uoreioxjjpiridLn-24uírboxamid; N^4-uinimv2»c{k!U|îrtïpii»4'OM>hînînO'UKH1"^«OiCîkiobuîUM-(.“<»^' í rü l u weíox I )pIkoIInan) Id ; N“[3“t2-;mimO''-Oxocùi)' U -dlaxotíetan-d-dj-d-* l-nucsruklohodlV 1-(*5SVM J-:-ifii1iuorpropan-2-ïi joxtpmd m-l-lprbpxasdd; N4342-PPiPo~2-bXônii)~t4-dsiÂ^ I·· flü*wcikiobutHípiridín-2-karbi>xanjid: I -eik lopropil" 1 -($*meUt-1,2,4-oxadiaxot-3-ii)etit)~5-{ 1-nuordk\ohaUÈ:HM 2,2,2- Irl ti uo re to x i 5 p i ko II « a nu d ; •’lEI-N^i-iáilopropil-l -(5-metil- i,2,4-oxadiaa>l~3-ü)«tflhS-{ I -fl«orciklob«tiî)-4~(2,2,2- trl OuoiPidxIlpíkóIdamídi Ν-»Β)-4-8ηϋηο-2-οΚΙ*'ΡΓορϋ^-ιν)Η»ΗΛθ-2-ιΊν5Ό^Η*ρη'ρΗ-4-Ηδν!'ίΐΡο?ρΓ0ρ3«^ lloxhpikohnamk!; ^d(l)->4'>am;lds>'2>élklopr(spil -4 .oxobutan-2 · H}-5-^ilöpropü-4-((S 5-1 -íluorprüpan~2* Hoxi)pikoHnanikí; M«((S M-amino-2-ciklopropiM-oxobuian-2-íl }-5-ciklopropií-4-({R}·· 1 -flüÉpGÉgHu^» iíoxAptkolinormd,. N-((R í-4 <smirtO:-2-elkl©pröpil"4-oxöfeuMn^2>ll)-5-elklppropil -4 -íí fl}-1 -{1uorpropan-2-iloxijpikoünamid; N-[{2S)-4“;anino-2-c!kk>proplk4'ítM'á3ü|8fS''2“ín”5-f l -fi uordklobui j l)-4-t 2,2,2-tnfiaórctox i)piridin-2-karboxarn ki ; és H ~ [ (22 Ií: ^ίΐΓΐΐ 1st ti >^c 1 fe í <>ppoíp 11 0 b íí i î ] s- S1 s> r^i Itl obiit 11} - 4 ~(2 s 2 '' $ rí Π uorc i ο X l>pl rkl in-2 - karboxu m k!.
  8. 15, Ap 1-14. igénypontok lépplyike «pdrlnirvegypjpk amely a kővetkezők közöl kiválasztva: 54IiklopropÍ!~4~(2,2t24íinuor"eisvKÍ}"piridín~2~karbon55av--|{R).'2'CÍkk>propn'-I"meül' i~ (S-meíií-i1,2.4|osadiazol“3'M}-ÄI-äpidt 5-ciklopropiM»((Sî»2s2,2-trinuor^'rnciit"eioxi)”pirk1in*2-kart>oniâav~[2“meuinsï:ulf{.înil·· I -mat; Μ »(3 -meiü- [ 1 ;2,4jo.x ad iazoI--3-11 H't'dj-amíd; 5--{3J--Dinuor--azeddin-I-íi)-4-'((S)--2;2<2--fríÍoP--l--Íp®tiI''eíOM|-fMdí?^2--kafl'OdkáPf2>-Melànsz«lfonU~Î-«ïiÂ41^5*mciU-| 1 >2»4)<.vKadiaa?.o!“3-i{}-eíiíj -amid; S --Ciki obup 1-4-(2,2,2 “írílluor-'öPxl }-p (idddt-2 -kaÉsodsav -42--dkí -metál ~JNf Sí rnod ! -{1,2,4]oxad íazol-3-i I)-eű; j-aro ki ; 3-eikÍ0h«íiM'--(2s2J~tnfe0r-ei0Mf-f§pdms2^^ meid -11,2,4}ö3íadMd! -3 >4Í}--eí í ! ]-ám ki; 5~olkk4)uiii'4-((SV2 3J-inn»ur-i-«iPi-êl0Xî>-pirid|P^ 41 ~ I 5 e tkl -1 : í : i ox ad i jsísoÍ" 3 - fl | a?ri i íi ; metaasxtdibnií-1 --meu I-1 -{S-rne-ut-j i ^sdljpiadippii-S-'lll-sidll-aKddj J-mtkldpeopi i-N-j. I -cik íopropu--2--(S4bdÉi-1 ;2,4>Mááí|^oí^*!i'}i3Mjp6a*2 - i i 1- 4 ..(2 „2. dk]uorctoai)piridín-2-karboxasvdd; 5'-0Ík:iopropll--l4-p:-áikÍopropli-3-(S-mdii:í-],2í4-Ps:sdisa0Í-'3-d)prPpad-2-sl'|-4-(2“ flui>r«toxí)p! ndín-2 --karboxamid; 5-0ÍkiopropiÍsN-j(2S)“i-cikíopropM-2-(5söípd^ls;2,4-öx:adiazol-3'lií|própap~2'-ÍÍÍ~4-(2,3-- difIuoretoxí)p5ridin-'2-vkafhPKamidj 5-cíkiopropí l-N-j (2$) - ! - c i ki opmp i k2 -· ( S-nted ! - i j2,4-madíazoi-3-íi|pr0pap^2-íl|-4-{2-íluoretoxí }pl rld m-2~karbox amid; :M-|3“(2^í«mö'-2"Oxotítil)'i, l"dioxoüetan-.3-d]-5-cikíop?'opü-4-(2,2,2-trvfl uorcioxl)p irkJm -2-karboxanuű; S^tklopropUdd^l^tklopropildHSonettM JAoxadiazoKR îl)pw>pan-2-ilpl· (2^,2*uif1uomoxi)pirklin"2"karbox8mid; 5-<ΐ1!νΙορΓοριΙ-Η'<[(28}~1-ο^|ορΐτ?ρΙ1-2-(5~ω6ΐΗ~1354'·οχΜ®20ΐ-2-'Π)ρΓ0ρ&amp;π»·2»ίΙ1·4'·(2ϊ2ί2- trinuoreíoxi)píndhi~2*karboxímú4f N-(4-á:mirK3"2~elk!öprDpíl4-0X0feiitan-2"il)>'S-cikiopropíl~4'>(2J2,2--tfsíluóreto>íi}pÍrsíiü'5~2'· karboxamid; Ni'(4-8nisn0''2-0Íkl0pr0p?!4-'0X0b0iá0-2-4l)''S“eiklopmpiÍ'4'-[{2S)~L:!5l“trifiíüorpropan~2~ i I |oxí pl r id m-2~kar boxam i d ; N'i4''amiiio^2''elk!opropll:^ “Oxobuton~2~t!}"S~vsk!opn>pi:l~4'-[pS}·' 1,1 > 1 ^dtluotpropan^ il jôxlpïr I d iîi-Ξξ í<f ; N43H2-'smbíO''2--0X0etíl}--Ll ''dä0X0detan-3s-41]-5~eiklöpröplk4“[(2S}'22l5l4Hflu0^r0pai0 23 ! Joxlp i ndin-24.arbt.>xam i d; NidX2R}^4'^lpp-2-0ikfopröpb^~oxobtdap^2dlj''5''Cíklopmpík4~(2't1uore0-xiíplrldk02·' kárboxámid; Kí>|;(2R)'-4-aaíHn0''-2”0Íkl0propíÍ^4"0xx2)utan"2“íi]*5-vikÍ0proiyO-4-(2s2'-dÏfiöorcuïXi.)plridínO- !>arboxatnid; és 2*ο1ΜορΓ0ρΙί~4'({8)~Ι.~ίΐ0θψΓ0ρ8Γΐ-2-4ΙοχΙ)~Ν·'({2}''2->{5·'ΐηβΙίΙ-'1,2>4K>xadiaxöÍ4M]}-'i"· {«íetiísaiddond íprop0n-2-y0plkolh:M«nkk 14. kijárás az 1-45. igénypontok bármelyike szerinti vegyület előáll kásám,, amely tartalmazza (B) képlett! vegyület reakcióját
    NBR'!ll2 amid kapcsolószer és bázis jelenlétében, ahol R*~R4 jelentése a Ibnii 1-13 igén ypontok hám?elvi keben meghatárazott*. 1/. Az I 15. igénypontok bármelyike s/cmui vegyidet terápiásán aktív anyagként történő alkalmazásra,:: II; A%, 1-41.- igénypontok bármelyike szerimt vegyöieteí és gyógyászati lag közdmhós hordozóanyagot tartalmazó gyógyszerkóSísltíMim 19. A7. I 15. igénypontok bármelyike szerintl vegyidet az alábbiak kezelésében vagy niegelözésébeu törtenó alkalmazásra:: fajdalom, áterosaklérózis, korrá! ossMÜggö makuiadegeneráeió, diabéieszes retmopaiia* zóídhályog, retinavéna elzáródás;, koraszülött reiínopátia, «kaláris iszkémiás szindróma, geográilás atróüa, diabetes mellitus, gyulladás, gÿidiadâsos bélbetegseg* tszkémiás-reperfuzíós sérülés, akut m^elégielenség, májfibrózás, didiibrSzia, veseibrizi, szisztémás fibrózis, akut állograt kilökődés, krónikus aitograf nefropáiia, diabetikus nefropáiia, glomeruionefropáila, kardiomiopáíia, szívelégtelenség, miökardiáíis iszkemra, mlokariláils infarktus, szisztémás szklemzis, ko okozta sérdiés, égés, hipemöMs hegek, keloiiok, glngivitisz plrexla, mfydrrézis vagy tumorok, esonttonmir Szabályozás, neurodegénéráétő, nmiotrótlás lateráfia szklerókls, szírok, átmeneti iszkén-ilás toliam vagy uvsibsz.
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